Captopril Floating and/or Bioadhesive Tablets: Design and Release Kinetics

Nur, Abubakr O.; Zhang, Jun S.

doi:10.1081/ddc-100101323

Cited by 87 publications

(55 citation statements)

References 16 publications

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“…However, the effect of the polymer Badam gum was more pronounced than HPMC K4 M on bioadhesion strength since Badam gum has significant sticking property these findings are in agreement with previously reported results by Meka, et al, [23] who found the Badam gum has remarkable swelling and sticking character in gastric pH. [23][24][25][26][27][28][29][30][31][32][33] This developed floating-bioadhesive combination formulation would overcome the drawback of floating and bioadhesive individual system and improving the therapeutic effect of the drug involved.…”

Section: Bioadhesive Strengthsupporting

confidence: 82%

“…Based on the R 2 -value, shown in Table 9 the best-fit model was selected. [32,33] Selection of optimized batch Selection of optimized batch is done on the basis of its drug release profile, in vitro buoyancy study, in vitro bioadhesion study, and floating lag time. [34,35] Stability study Stability study was conducted according to ICH guidelines at 40±2°C and 75±5% RH for 6 months.…”

Section: Kinetic Modeling Of Drug Releasementioning

confidence: 99%

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Nawaj¹

2017

AJP

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Aim: The objectives of this investigation were to develop gastroretentive floating bioadhesive drug delivery for simvastatin to increase gastric residence time and reduce the dose frequency. To explore Badams gum's sticking property in floating bioadhesive drug delivery of simvastatin. Materials and Methods: Floating bioadhesive tablet was formulated with Badam gum and hydroxypropyl methylcellulose (HPMC) K 15 M polymers, sodium bicarbonate, and citric acid as the gas generating agents to reduce floating lag time. Tablets were prepared by direct compression method. Optimization study was conducted using 3 2 factorial design. The concentration of polymers was considered as independent variables whereas swelling index, bioadhesive strength and % drug release at 10 h, of the tablets were utilized as dependent variables. Results and Discussions: Preformulation study suggests powders blends shows acceptable flow properties. Simvastatin floating-bioadhesive tablet found to be good without chipping, capping, and sticking. Comparing all the formulations, A5 optimized formulation exhibited 98.10 ± 2.10% of drug release in 12 h, floating lag time of 34 ± 3 s, with appropriate bioadhesive property, and total floating time of over 12 h. It was observed that increasing percentage of polymer in formulation the drug release decreased. Developed formulations were stable during stability studies. Conclusion: Based on these findings, it was concluded that Badam gum can be used as a bioadhesive as well as release retarding polymer for the floating bioadhesive dosage form of other drugs.

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Section: Bioadhesive Strengthsupporting

confidence: 82%

Section: Kinetic Modeling Of Drug Releasementioning

confidence: 99%

Untitled

Nawaj¹

2017

AJP

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“…The mean and deviation was determined. The percent deviation was calculated using the following formula 14 .…”

Section: Evaluation Of Tablets Weight Variation Testmentioning

confidence: 99%

Formulation and in Vitro Evaluation of Simethicone Tablets as Gasrto Retentive Drug Delivery System

Mangilal¹,

Rao²

2017

Int. Res. J. Pharm.

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ABSTARCTThe aim of the present study was to develop a delayed release formulation of Simethicone to maintain constant therapeutic levels of the drug for over 12 hrs. Various grades of HPMC polymers and accrual were employed as polymers. Simethicone dose was fixed at 62.5 mg. The total weight of the tablet was considered as 300 mg. Polymers were used in the concentration of 10, 20 and 30 mg concentration and accrual concentration used in the formulations were optimized according to the floating properties of the formulations. All the formulations were passed various physicochemical evaluation parameters like hardness, bulk density, friability, weight variation etc. and they were found to be within limits and also the drug and excipient studies showed that there is no incompatibility between pure drug and excipient. Whereas from the dissolution studies, it was evident that the optimized formulation (F6) showed better and desired drug release pattern i.e.,98.17 % in 12 hours. The optimized formulation dissolution data were subjected to release kinetics; from the release kinetics data it was evident that the formulation followed Higuchi mechanism of drug release.

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“…As the pH increases, CAP becomes unstable and undergoes degradation. 2,3 CAP has been a drug of choice in hypertension management; however, its antihypertensive action is effective for 6-8 hours, which is why three to four CAP administrations are required for successful medication. Therefore, development of a controlled delivery system for CAP would bring many advantages for hypertension patients, who compose almost 25% of the world's population.…”

Section: Introductionmentioning

confidence: 99%

New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

Azevedo¹,

Tasic²,

Fattori³

et al. 2011

IJN

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Captopril (CAP) was the first angiotensin I-converting enzyme (ACE) inhibitor to be developed and is widely used in hypertension treatment. On the other hand, cyclodextrins (CDs) are cyclic oligosaccharides whose cone-shaped cavity allows formation of noncovalent inclusion complexes with appropriately sized guest molecules, thus modifying guest physical, chemical, and biological properties. Herein, the physicochemical characterization and in vivo ACE inhibition evaluation of seven CAP/CD complexes are reported. The inclusion complexes were prepared by spray-drying, freeze-drying, kneading, or lyophilization methods and characterized by nuclear magnetic resonance, Fourier-transformed infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy techniques. In vivo assays compared CAP and CAP/CD complex administration (0.5 mg kg −1 or 0.09 mg kg −1 , n = 4–7) to evaluate the ACE inhibition by continuous infusion of angiotensin I (30 ng 50 μL −1 min −1 ) in conscious Wistar rats. The physicochemical analysis demonstrated complete amorphization and complexation between CAP and CDs, indicating the substitution of water molecules inside the CD cavity with CAP. During the infusion of angiotensin I, the administration of all CAP/CD complexes induced a reduction in mean arterial pressure similar to that observed upon CAP administration. The nanoparticles obtained by the kneading method (CAP/α-CD:KM) showed a potent and long-lasting inhibitory activity (∼22 hours) on the angiotensin I pressor effect. The results suggest that the inclusion complex of CAP and α-CD can function as a novel antihypertensive formulation that may improve therapeutic use of CAP by reducing its oral dose administration to once per day, thus providing better quality of life for almost 25% of the world’s population who suffer from hypertension.

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Captopril Floating and/or Bioadhesive Tablets: Design and Release Kinetics

Cited by 87 publications

References 16 publications

Untitled

Untitled

Formulation and in Vitro Evaluation of Simethicone Tablets as Gasrto Retentive Drug Delivery System

New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

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